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Palonosetron

  • Lee SchwartzbergEmail author
Chapter

Abstract

With the recognition that the 5-hydroxytryptamine receptor was important in mediating cisplatin-induced emesis, work at several pharmaceutical companies focused on creating drugs that interfered with serotonin binding utilizing a variety of medicinal chemistry strategies. The first-generation 5-hydroxytryptamine receptor antagonists (5-HT3 RAs) ondansetron, granisetron, tropisetron, and dolasetron were structurally similar and showed activity in preventing chemotherapy-induced nausea and vomiting. However, complete response during the acute phase after cisplatin was achieved in only 50–70 % of patients and was substantially less effective in the delayed phase for control of both emesis and nausea. The first-generation 5-HT3 RAs do not improve control of delayed CINV over dexamethasone alone [1], nor does prolonged administration provide much additional benefit [2]. In addition, the first-generation 5-HT3 RAs were therapeutically equivalent with several large trials comparing these drugs to one another demonstrating similar efficacy [3, 4]. A plateau in 5-HT3 RA activity had been reached. Efforts persisted to find potentially more active agents based on the understanding of the central importance of this specific serotonin receptor in ameliorating chemotherapy-induced emesis.

Keywords

Complete Response Rate Moderately Emetogenic Chemotherapy Palonosetron Group CINV Prophylaxis Moderately Emetogenic Chemotherapy Regimen 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Springer International Publishing Switzerland 2016

Authors and Affiliations

  1. 1.Division of Hematology/Oncology, Department of MedicineUniversity of Tennessee Health Science CenterMemphisUSA

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